Species

diazepam

Summary

Summary: A benzodiazepine with anticonvulsant, anxiolytic, sedative, muscle relaxant, and amnesic properties and a long duration of action. Its actions are mediated by enhancement of GAMMA-AMINOBUTYRIC ACID activity. It is used in the treatment of severe anxiety disorders, as a hypnotic in the short-term management of insomnia, as a sedative and premedicant, as an anticonvulsant, and in the management of alcohol withdrawal syndrome. (From Martindale, The Extra Pharmacopoeia, 30th ed, p589)

Top Publications

A detailed ethological analysis of the mouse open field test: effects of diazepam, chlordiazepoxide and an extremely low frequency pulsed magnetic field

..formation, but do not do so uniformly, with a maximum amnesic effect after lorazepam but less or no effect after diazepam, we were interested in testing in this non-behavioural study to what extent the effects of lorazepam and diazepam ..

A case with atypical childhood occipital epilepsy "Gastaut type": an ictal migraine manifestation with a good response to intravenous diazepam

..three anxiolytic drugs from two different chemical and pharmacological classes: buspirone, chlordiazepoxide and diazepam. When the test tank was novel the diving response was clearly seen whereas it was significantly reduced when the ..

Comparison of the interaction potential of a new proton pump inhibitor, E3810, versus omeprazole with diazepam in extensive and poor metabolizers of S-mephenytoin 4'-hydroxylation

..In this study, we evaluated (18)F-FDG uptake in BAT of rats to determine whether pharmacologic or physiologic interventions affect the uptake, knowing that BAT has a high density of adrenergic innervation...

Effects of diazepam on gene expression and link to physiological effects in different life stages in zebrafish Danio rerio

We applied zebrafish whole genome microarrays to identify molecular effects of diazepam, a neuropharmaceutical encountered in wastewater-contaminated environments, and to elucidate its neurotoxic mode of action...

Risk of fractures requiring hospitalization after an initial prescription for zolpidem, alprazolam, lorazepam, or diazepam in older adults

..By using multiple homology models and an unbiased docking protocol, we identified a binding hypothesis for the diazepam-bound structure of the benzodiazepine site, which was confirmed by experimental evidence...

Unraveling the metabolic transformation of tetrazepam to diazepam with mass spectrometric methods

Mice with point-mutated alpha2 GABA(A) receptor subunits (rendering them diazepam insensitive) are resistant to the anxiolytic-like effects of benzodiazepines (BZs) in the conditioned emotional response (CER) test, but show normal ..

Interaction between cannabinoid compounds and diazepam on anxiety-like behaviour of mice

The benzodiazepine agonist, diazepam, inhibits cAMP production in the rat brain. Since cAMP influences c-fos activity, we examined the effects of diazepam on expression of this immediate early gene, as indicated by Western blot analysis...

..of seizure activity following exposure to the nerve agent soman (GD) includes treatment with the anticonvulsant diazepam (DZP), an allosteric modulator of γ-aminobutyric acid A (GABA(A)) receptors...

..Here, we report a patient with severe NMS who was successfully treated with highdose lorazepam and diazepam. A 61-year-old man with bipolar I disorder was admitted to the hospital because of manic episodes...

..an anticholinergic drug and an acetylcholinesterase reactivator, is often completed with the anticonvulsive drug diazepam to prevent poisoned organisms from centrally mediated seizures and subsequent tonic-clonic convulsions...

..The aim of this study was to determine whether intranasal midazolam is as safe and effective as intravenous diazepam in the treatment of acute childhood seizures...

Differential effects of MPEP and diazepam in tests of conditioned emotional response and Pavlovian-to-instrumental transfer suggests 'anxiolytic' effects are mediated by different mechanisms

S A GeorgeDepartment of Psychology, School of Life Sciences, University of Sussex, Falmer, Brighton, UKPsychopharmacology (Berl) 204:499-509. 2009

..The standard test of the ability of Pavlovian cues to motivate responding is the Pavlovian-to-instrumental transfer (PIT) paradigm and it has recently been suggested that CER may be 'negative PIT'...

Ethanol effects on impulsivity in two mouse strains: similarities to diazepam and ketamine

..The effects of ethanol on attention and impulsivity have been contradictory...

Acute and chronic effects of the synthetic neuroactive steroid, ganaxolone, against the convulsive and lethal effects of pentylenetetrazol in seizure-kindled mice: comparison with diazepam and valproate

..3 or 4 x LD(50) of soman could not be terminated unless an adjunct therapy consisting of procyclidine (6 mg/kg), diazepam (10 mg/kg), and pentobarbital (30 kg/kg) was given, and the mortality rate was comparatively high (78%)...

..Using mice, which carry a point mutation that renders specific subtypes of GABA A receptors diazepam insensitive, it was recently discovered that particular types of GABA A receptors are involved in specific, ..

Effects of benzodiazepines receptor agonists on the hypothalamic-pituitary-adrenocortical axis

..anxiolytic, muscle relaxant, anticonvulsant and cognition-impairing effects of clinically used BZs such as diazepam. We created genetically modified mice (alpha1 H101R) with a diazepam-insensitive alpha1 subtype and a selective ..

Modulation of passive avoidance in mice by the 5-HT1A receptor agonist flesinoxan: comparison with the benzodiazepine receptor agonist diazepam

..agonist flesinoxan on passive avoidance in mice were compared with those of the benzodiazepine receptor agonist diazepam. In preliminary experiments, the retention latency to enter a dark compartment in mice subjected to single-..

The aim of the present study was to investigate the feasibility of the inclusion of a water-insoluble drug (diazepam, DZ) into solid lipid nanoparticles (SLNs), which offer combined advantages of rapid onset and prolonged release of the ..

..To clarify whether this effect is due to central or peripheral mechanism, we administered 5 mg of diazepam or saline intravenously to healthy volunteers and assessed the change in blood pressure, heart rate, muscle ..

..Recent evidence implies that the processing of different facial expressions may also be dissociable pharmacologically by GABAergic and noradrenergic compounds, although no study has directly compared the two types of drugs...

Requirement of alpha5-GABAA receptors for the development of tolerance to the sedative action of diazepam in mice

Zolpidem and diazepam are widely used drugs acting via benzodiazepine binding sites on GABA(A) receptors. While diazepam is non-selective, zolpidem has a high affinity for alpha1-, and no affinity for alpha5-containing receptors...

Different neuroprotection and therapeutic time windows by two specific diazepam regimens on retinal ganglion cells after optic nerve transection in adult rats

..To address this situation, we investigated the biotransformation potential of diazepam in primary porcine hepatocytes with a flat membrane bioreactor (FMB); we used human plasma exposure and serum-..

Sex-specific effects of in utero manipulation of GABA(A) receptors on pre- and postnatal expression of BDNF in rats

Exposure to diazepam (DZ) during the last week of in utero development in rats induces neurobehavioral effects that do not become apparent in exposed animals until young adult ages. Some of the effects are sex specific...

It has been reported that Ginkgo biloba extract (GBE) is an inducer or inhibitor of microsomal cytochrome P450 (CYP) 2C19, and diazepam is a substrate of CYP2C19. Thus, it could be expected that GBE may alter the metabolism of diazepam.

Detection of aneuploidy in rodent and human sperm by multicolor FISH after chronic exposure to diazepam

..From these findings, a rebound phenomenon in terms of sleep latency was confirmed with etizolam and triazolam in rats. Furthermore, the 5-HT(1A) agonist, tandospirone, caused no rebound phenomenon regarding sleep latency in rats...

A higher inherent trait for fearfulness is associated with increased anxiety-like behaviours and diazepam sensitivity in Japanese quail

..We describe here such proximity-accelerated chemical coupling reactions of alpha(1)S205C and alpha(1)T206C with a diazepam derivative modified at the C-3 position with a reactive isothiocyanate group (-NCS)...

Diazepam-induced disruption of classically-conditioned fear-potentiation of late-latency auditory evoked potentials is prevented by flumazenil given before, but not after, CS/US pairing

..Recently we reported that the N1/P2 auditory evoked potential was enhanced by fear conditioning in humans. Diazepam 10 mg, given before CS/US pairing, prevented subsequent expression of fear potentiation when the response was ..

The role of diazepam in the treatment of nerve agent poisoning in a civilian population

The main site of action of diazepam, as with other benzodiazepines, is at the GABA(A) receptor, although it has been suggested that some of the potentially beneficial actions of diazepam in nerve agent poisoning are mediated through other ..

To compare the efficacy and tolerability of buccal midazolam with rectal diazepam as emergency treatment in residential adults with convulsive or non-convulsive serial seizures or status epilepticus (SE), and ascertain the preference ..

Two compartment model of diazepam biotransformation in an organotypical culture of primary human hepatocytes

..limitation, we used an organotypical model of human primary hepatocytes for the biotransformation of the drug diazepam with special reference to metabolites in both the cell matrix phase and supernatant and its interaction of three ..

Effects of the aqueous extract from Salvia miltiorrhiza Bge on the pharmacokinetics of diazepam and on liver microsomal cytochrome P450 enzyme activity in rats

..with Tween 80 as surfactant, propylene glycol and ethanol as cosolvents was developed for intranasal delivery of diazepam. Phase behavior and solubilization capacity of the microemulsion system were characterized and in vivo nasal ..

..inhibited AChE;2) atropine to antagonize the action of excess acetylcholine formed at muscarinic receptors and 3) diazepam or midazolam to allosterically potentiate the action of inhibitory neurotransmitter -amino butyric acid (GABA) at ..

..of [unreadable]II-spectrin, a calpain substrate, to document calpain I activation;(5) parentera administration of diazepam and phenobarbital after METH administration to stop electrographic seizures, which we predict will also provide ..

..These effects are reminiscent of detrimental behavioral effects observed upon treatment of young mice with diazepam, a prototype benzodiazepine that potentiates the function of GABA via GABA-A receptors...

..AChE) reactivator pralidoxime (2-[(hydroxyimino)methyl]-1-methylpyridinium, 2-PAM), and symptom modulator diazepam. From a single intramuscular (IM) dose these compounds do provide some immediate protection, but for persistent ..

..The ?2-containing GABAA receptors, which have been shown to mediate the anxiolytic-like action of diazepam in ethological tests of anxiety will be deleted from hippocampal principal neurons in the CA1, CA3, and DG ..

..To develop a drug therapy for catamenial seizure exacerbation, we will examine two drugs, diazepam and the "neuroactive steroid" ganaxolone, using a 2-day pulse-therapy protocol for two withdrawal cycles...

..genetic and pharmacological approach to create a model system (triple point-mutated mice + the non-selective drug diazepam) in which diazepam is a true ?1-specific, ?2-specific, ?3-specific, or ?5-specific full agonist, respectively, ..

..A second portion of the proposed experiments will test for tolerance to the discriminative stimulus properties of diazepam. There is surprisingly little information available about this type of tolerance, and the proposes studies will ..

..Both the impairment of maze learning and LTP inhibition can be prevented by pretreatment with losartan. Because diazepam produces similar effects and these effects can also be prevented by pretreatment with losartan, we also assume ..

..to further delineate behavioral and pharmacological variables that contribute to the reinforcing properties of diazepam and to investigate the discriminative stimulus (DS) properties and subjective effects of diazepam...

..In a pilot study mass selection was used to breed divergent lines of mice which are resistant and sensitive to diazepam (DZ). Mice were selected for mating based on the duration of impairment on the rotarod (i.e...

..ligands can selectively attenuate measures of ETOH reinforcement; this may be related to their binding at diazepam sensitive (DS), and to a lesser degree at diazepam insensitive (DI) conformations of GABAA-BDZ receptors...

..ligands can selectively attenuate measures of ETOH reinforcement; this may be related to their binding at diazepam sensitive (DS), and to a lesser degree at diazepam insensitive (DI) conformations of GABAA-BDZ receptors...

..will be antagonized by flumazenil and whether this treatment results in an increase in mRNA expression for diazepam binding inhibitor (DBI), an endogenous BZD-inverse agonist, allowing identification of brain sites where adaptive ..

..treatments include systemic administration of the narcotics morphine and fentanyl, and of the benzodiazepine diazepam. Also included is presentation of a warning signal prior to application of the noxious stimulus...

..Our preliminary data from studies examining the acute effects of various benzodiazepines (diazepam, alprazolam, and lorazepam) on performance of cognitively intact normal volunteers suggest that possession of the ..

..present application is based on preliminary findings indicating that: 1) a single pretreatment with a low dose of diazepam significantly enhances the anticonvulsant effect of the same dose readministered two weeks later; 2) one ..

..a role in pathologic states of anxiety, our original study examined sensitivity to successive injections of IV diazepam in panic disorder patients and controls, using saccadic eye velocity as the major pharmacodynamic measure...